ABSTRACT
Chemical fractionation of the n-BuOH partition, which was generated from the EtOH extract of the flower buds of Tussilago farfara, afforded a series of polar constituents including four new sesquiterpenoids (1-4), one new sesquiterpenoid glucoside (5) and one known analogue (6) of the eudesmane type, as well as five known quinic acid derivatives (7-11). Structures of the new compounds were unambiguously characterized by detailed spectroscopic analyses, with their absolute configurations being established by X-ray crystallography, electronic circular dichroism (ECD) calculation and induced ECD experiments. The inhibitory effect of all the isolates against LPS-induced NO production in murine RAW264.7 macrophages was evaluated, with isochlorogenic acid A (7) showing significant inhibitory activity.
Subject(s)
Animals , Mice , Flowers/chemistry , Glucosides/pharmacology , Sesquiterpenes/pharmacology , Sesquiterpenes, Eudesmane/pharmacology , Tussilago/chemistryABSTRACT
OBJECTIVE@#To investigate the effecr of siRNA-interfering β-catenin expression on drug-resistance of multiple myeloma cells.@*METHODS@#The multiple myeloma cell line RPMI-8226 was cultured in vitro. The maphalan-resistant cell model was established by concentration gradient ascending of durg, then the drug-resistant cell line was instantaneously transfected with β-catenin siRNA, the sensitivity of RPMI 8226 cells to maphalan was detected by CCK-8 meltod before and after the transfection with siRNA; the mRNA and protein expression of β-catenin was detected by qRT-PCR and Western blot respectively, the apoptosis of cells was detected by flow cytometry.@*RESULTS@#IC of maphalan decreased from (5.29±0.19) μmol/L to (1.88±0.64) μmol/L, suggesting that the deplation of β-eatenin restored the sensitivity of drug-resistant cell line RPMI-8226 to malphalan. The Western blot showed that after the instaintaneous transfection with β-catenin siRNA, the β-catenin protein expression level obviously decreased, compared with level before transfection. After transfection, the maplalan-inducing apoptosis rate of cells increased from (35±0.5)% to (54±0.4)%, suggesting that the β-catinin gene may correlated with drug-resistance of cells. Interfering the expression of β-catenin gene could enhance the sensitivity of drug-resistant RPMI-8226 cells to maphalan.@*CONCLUSION@#The β-catenin siRNA interfereuce can inhisit the β-catenin gene expression in Wnt/β-catenin signaling pathway, suppress the cell proliferation, enhence the toxicity of maphalan on drug-resistant RPMI-8226 cells, thus result in increase of cell apoptosis.
Subject(s)
Humans , Apoptosis , Cell Line, Tumor , Cell Proliferation , Multiple Myeloma , RNA, Small Interfering , beta Catenin , GeneticsABSTRACT
OBJECTIVE@#To explore the effect of Bushen Yanggu Decoction (BYD) on drug resistance and proliferation of human multiple myeloma-resistant KM3/BTZ cells.@*METHODS@#Human multidrug-resistant KM3/BTZ cells were established by Bortezomib (BTZ) gradient induction. The effects of commonly used chemotherapeutic drugs and serum containing Bushen Yanggu Decoction (BYD) on the proliferation of KM3 cells and KM3/BTZ cells were detected by MTT assay. RT-qPCR and Western blot were used to detect the expression of Par-4, HSP27 and P-gp genes. Flow cytometry was used to detect cell apoptosis.@*RESULTS@#The established KM3/BTZ cells could produce varying degree of resistance to commonly used chemotherapeutic drugs. Among them, the highest resistance index (RI) to BTZ was 20.269. MTT assay showed that the proliferation of KM3/BTZ cells treated with serum containing Bushen Yanggu Decoction was inhibited, and the inhibitory effect increased with the serum concentration incranse of Bushen Yanggu Decoction. The serum containing Bushen Yanggu Decoction could inhibit the proliferation of KM3/BTZ cells, and induce apoptosis, significantly reduce the drug-resistance of KM3/BTZ cells, up-regulate the expression of Par-4, down-regulate the expression of HSP27 and P-gp.@*CONCLUSION@#Bushen Yanggu Decoction can effectively inhibit the proliferation of KM3/BTZ cells and induce apoptosis. Bushen Yanggu Decoction can effectively reverse the multidrug-resistance of KM3/BTZ cells. The mechanism may be related with the decrease of expression of HSP27 and P-gp and the increase of expression of Par-4.
Subject(s)
Humans , Apoptosis , Bortezomib , Cell Line, Tumor , Drug Resistance, Multiple , Drug Resistance, Neoplasm , Multiple MyelomaABSTRACT
Objective To study the chemical constituents from Bletilla ochracea. Methods The compounds were extracted by 95％ alcohol and isolated by column chromatography on silica gel and Sephadex LH-20. Their structures were identified by spectroscopic analysis (～1 H NMR and 13 CNMR).Results Nine compouds were obtained and identified as lusianthridin (1), 1, 2, 7-trihydroxy-4-methoxy-9, 10-dihydroxyphenanthrene (2), nudol (3), coelonin (4), batatasin Ⅲ (5), 3, 7-dihydroxy-2, 4-dimethoxyphenanthrene (6), daucosterol (7), β-sitosterol (8), stigmasterol (9).Conclus ion Compounds 2, 3, 5 were isolated from this plant for the first time.
ABSTRACT
Objective To study the bibenzyls and phenanthrenes from Arundina graminifolia.Methods The compounds were extracted by 95％ alcohol and isolated by column chromatography on silica gel and Sephadex LH-20.Their structures were identified by spectroscopic analysis (1H NMR and13CNMR).Results Eleven compouds were obtained and identified as batatasin Ⅲ (1),arundinanin (2),2,8-dihydroxy-4,7-dimethoxy-9,10-dihydrophenanthrene (3),shancidin (4),arundinan (5),isoshancidin (6),erianthridin (7),lusianthridin (8),eulophiol (9),flavanthrin (10),orchinol (11).Conclusion Compounds 3,7,9 were isolated from this plant for the first time.